Tyrosine Phosphatase Screening and Profiling Service
Creative Biogene provides multiple tyrosine phosphatases (PTPs) screening and profiling services to accelerate your research and drug discovery program. Our talented scientists with years of experience will offer specialized and fully defined services for screening potential modulators of PTP. As a pioneer in this field, we establish an efficient screening and profiling platform based on biochemical and cellular phosphatase assays. On this basis, we will assist you with the most affordable and high-quality service to ensure your satisfaction in a timely and professional manner.
Protein tyrosine phosphatase (PTP) is a kind of enzyme that remove phosphate groups from phosphorylated tyrosine residues on proteins. It is a signaling enzyme that, together with protein tyrosine kinase (PTK), regulates tyrosine phosphorylation inside the cell. Protein tyrosine phosphorylation is essential for the initiation, propagation, and termination of signal transduction in response to growth factors, hormones, cytokines, and cell−cell contacts. Aberrant tyrosine phosphorylation, resulting from alteration of PTP expression, misregulation and mutation, has been linked to the etiology of many human ailments including cancer, diabetes/obesity, autoimmune disorders and infectious diseases. Therefore, it becomes very important to screen effective and safe compounds in the discovery and development of targeted drugs. Some small-molecular compounds are reported as PTP modulators, which play an important role in targeted therapy area.
Table 1. Some small-molecule effectors of validated PTP drug targets
| PTPs | Effector | Targeted pathology |
| TC-PTP | Mitoxantrone | Cancer, diabetes |
| CDC25 | Vitamin K3-like quinone derivatives | Cancer |
| DEP-1 (R-PTPη) | Dimerizing peptide | Cancer |
| SHP2 (PTP-1D) | Sodium stibogluconate | Cancer |
| PTP1B | ISIS-PTP1BRx | Diabetes and obesity |
| PRL-3 | Thienopyridone and anthraquinones | Cancer |
| LYP | LTV-1 | Autoimmune diseases |
| CD45 | L158429, R164259, S349631 | Immune and inflammatory diseases |
| PTP-MEG2 | Phosphonodifluoromethyl phenylalanine
derivatives | Diabetes |
| PTEN | Bisperoxovanadate derivatives | Ischemia and reperfusion injury |
Creative Biogene offers a convenient way for customers to quickly identify novel PTP inhibitors or activators, by screening your compounds across any of PTP targets on our panel. We provide flexible service in several formats, including single point analysis, IC50 determination and high throughput screening for large numbers compounds. Our comprehensive PTP screening and profiling services will boost your capability in evaluating structure-activity relationship in drug development process and minimize the risks in overall clinical stage.
Service highlights:
- High throughput screening including FP-based assay and FRET-based assay.
- Fast turnaround time
- Highly customizable
- Over 20 PTP target assays
Table 2. PTP screening targets
| Non-receptor PTP | Receptor PTP | dual-specific phosphatase |
| PTP1B | CD45 | PRL-1 |
| TC-PTP | LAR | PRL-2 |
| SHP2 | DEP1 | PRL-3 |
| MEG2 | RPTP | MAP1 |
If you have any requirements in tyrosine phosphatase screening and profiling services, please feel free to contact us. We are looking forward to working together with your attractive projects.
References:
- Sotoud, H. et al. (2013). Development of a colorimetric and a fluorescence phosphatase-inhibitor assay suitable for drug discovery approaches. Journal of Biomolecular Screening, 18(8), 899-909.
- Sofie De, M. (2012) ‘Challenges and Opportunities in the Development of Protein Phosphatase-Directed Therapeutics’, ACS Chem. Biol., 8, 36−4
* For research use only. Not intended for any clinical use.